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Assay Detail

CHEMBL4013289

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human complement factor D catalytic domain (G24 to A253 residues) expressed in expressed in Escherichia coli(Rosetta) using cobra venom factor-factor B complex as substrate preincubated for 1 hr followed by substrate addition measured after 1 hr by ELISA
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Complement factor D (CHEMBL2176771)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J.
J Med Chem (2017) 60 : 5717 -5735
PubMed 28621538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.39 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4065529 1 6.68
CHEMBL3908849 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4065529 IC50 = 210.0 nM 6.68
CHEMBL3908849 IC50 = 800.0 nM 6.10